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Compound Detail

CHEMBL315788

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COc1ccc(-c2nn(CC3CCCCC3)c(C(=O)O)c2Cc2cc3c(cc2Cl)OCO3)cc1

Basic Information

ChEMBL ID CHEMBL315788
Phase Preclinical
Structure Type MOL
InChI Key RMWPSJXRIZVXFS-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

483.0
MW (Da)
5.81
ALogP
6
HBA
1
HBD
82.8
PSA (Ų)
0.46
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H27ClN2O5
MW 482.96
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.71

Activity Summary

IC50 2 meas. best 6.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin receptor type B
CHEMBL4631
IC50 6.75 6.75 178.0 1
Endothelin-1 receptor
CHEMBL4566
IC50 5.64 5.64 2300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11086733 10.1016/s0960-894x(00)00513-8 Endothelin-1 receptor 1
11086733 10.1016/s0960-894x(00)00513-8 Endothelin receptor type B 1

Data from ChEMBL 36 via Core Engine